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Gamma-aminobutyric acid, a GABA-B receptor agonist. A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1] There are three receptors of the gamma-aminobutyric acid. The ...
A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms , pain , and hyperreflexia . The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics .
A GABAergic or GABAnergic agent is any chemical that modifies the effects of GABA in the body or brain. Some different classes of GABAergic drugs include agonists, antagonists, modulators, reuptake inhibitors and enzymes. [1]
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures [10] [7] of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. [11]
Despite the fact that gabapentinoids are GABA analogues, gabapentin and pregabalin do not bind to GABA receptors, do not convert into GABA Tooltip γ-aminobutyric acid or GABA receptor agonists in vivo, and do not modulate GABA transport or metabolism. [15] [16] Conversely, GABA does not bind appreciably to the α 2 δ protein. [17]
This mechanism is responsible for the sedative effects of GABA A allosteric agonists. In addition, activation of GABA receptors lead to the so-called shunting inhibition, which reduces the excitability of the cell independent of the changes in membrane potential. There have been numerous reports of excitatory GABA A receptors.
Pregabalin is not a GABA A or GABA B receptor agonist. N-Type Voltage-gated calcium channel. There are two drug-binding α 2 δ subunits, α 2 δ-1 and α 2 δ-2, and pregabalin shows similar affinity for (and hence lack of selectivity between) these two sites. [31]
Gaboxadol is a supra-maximal agonist at α 4 β 3 δ, low-potency agonist at α 1 β 3 γ 2, partial agonist at α 4 β 3 γ, and antagonist at ρ1 GABA A receptors. [5] [6] [7] Its affinity for extrasynaptic α 4 β 3 δ GABA A receptors is 10-fold greater than other subtypes. [8]